9-硝基喜树碱脂质体的释放度研究

 目的考察影响9-硝基喜树碱脂质体释放度的因素。方法采用薄膜-超声法制备了9-硝基喜树碱脂质体。建立了利用高效液相色谱法测定药物释放度的方法,并考察了水合介质渗透压、水合介质pH、胆固醇比例和脂质体粒径等处方因素对脂质体释药的影响。结果9-硝基喜树碱从脂质体中的释放过程符合Higuchi方程。水合介质渗透压、胆固醇比例和脂质体粒径对脂质体的释放度都有显著影响,但水合介质pH的影响不大。结论处方因素可以影响9-硝基喜树碱脂质体的释放度,有必要对这些影响因素进行控制以保证脂质体的缓释效果。

Research on Release Profile of 9-Nitrocamptothecin Liposome

OBJECTIVE To investigate the effects of factors on drug release from 9-nitrocamptothecin(9-NC) liposome.METHODS 9-NC liposome was prepared by film dispersion-sonication method.The drug release profiles were determined by validated HPLC method.The effects of osmotic pressure of hydrating medium,pH in hydrating medium,cholesterin proportion and particle size of liposome on drug release were investigated.RESULTS The releasing process of 9-NC from liposome followed Higuchi equation.The release profiles were influenced by the osmotic pressure of hydrating medium,cholesterin proportion and particle size of liposome.However,pH in hydrating medium had a little effect on release rate.CONCLUSION The release profile of 9-NC from liposome in vitro is significantly influenced by some formula factors.These factors should be controlled to ensure the sustained release effect of liposome.